Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAY1217389 是一种有效的选择性单极纺锤体 1 (MPS1) 激酶抑制剂 ,IC50值小于10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 333 | 现货 | ||
2 mg | ¥ 482 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,130 | 现货 | ||
50 mg | ¥ 3,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 863 | 现货 |
产品描述 | BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM). |
靶点活性 | Mps1:<10 nM |
体外活性 | In biochemical assays, the IC50 value of BAY 1217389 is 0.63±0.27 nmol/L. It shows high selectivity against other kinases and found to bind to PDGFRβ (<10 nmol/L), Kit (between 10 and 100 nmol/L), CLK1, CLK2, CLK4, JNK1, JNK2, JNK3, LATS1, MAK, MAPKAP2, MERTK, p38β, PDGFRα, PIP5K1C, PRKD1, and RPS6KA5 (between 100 and 1,000 nmol/L). In cellular mechanistic assays, BAY1217389 abrogats nocodazole-induced SAC activity and induced premature exit from mitosis ('mitotic breakthrough'), resulting in multinuclearity and tumor cell death. It is found to inhibit cell proliferation with a median IC50 of 6.7 nmol/L (range 3 to >300 nmol/L)[1]. |
体内活性 | In vivo, BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. Its blood clearance is found to be low in the tested species. Vss is high and terminal half-lives were long. BAY 1217389 is administered orally to female NMRI mouse (1 mg/kg) and male Wistar rat (0.5 mg/kg). Peak plasma concentrations are observed between 1.5 and 7 hours. Oral bioavailability is high in rat and moderate in mouse[1]. |
激酶实验 | Inhibition of recombinant human Mps1 by BAY 1161909 or BAY 1217389 is assessed in TRFRET-based in vitro kinase assays via phosphorylation of a biotinylated peptide (Biotin-Ahx-PWDPDDADITEILG-NH2). Under standard assay conditions kinase and test compound are preincubated for 15 min before enzyme reaction is started by addition of substrate and ATP upon 10 μM[1]. |
细胞实验 | Cells are seeded into 96-well plates at densities ranging from 1,000 to 5,000 cells per well in the appropriate medium supplemented with 10% FCS. After 24 hours, cells are treated in quadruplicates with serial dilutions of compounds. After further 96 hours, adherent cells are fixed with glutaraldehyde and stained with crystal violet. IC50 values are calculated by means of a 4-parameter fit using the company's own software.(Only for Reference) |
分子量 | 561.5 |
分子式 | C27H24F5N5O3 |
CAS No. | 1554458-53-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (165.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL (5.34 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.7809 mL | 8.9047 mL | 17.8094 mL | 44.5236 mL |
5 mM | 0.3562 mL | 1.7809 mL | 3.5619 mL | 8.9047 mL | |
DMSO | 10 mM | 0.1781 mL | 0.8905 mL | 1.7809 mL | 4.4524 mL |
20 mM | 0.089 mL | 0.4452 mL | 0.8905 mL | 2.2262 mL | |
50 mM | 0.0356 mL | 0.1781 mL | 0.3562 mL | 0.8905 mL | |
100 mM | 0.0178 mL | 0.089 mL | 0.1781 mL | 0.4452 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BAY1217389 1554458-53-5 Cytoskeletal Signaling Kinesin Inhibitor BAY 1217389 Mps1 BAY-1217389 Monopolar spindle 1 inhibit inhibitor